Metrogil - instructions for use, dose, side effects, contraindications

Antiprotozoal and antimicrobial drug, a derivative of 5-nitroimidazole. The mechanism of action is the biochemical reduction of the 5-nitro group of metronidazole by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group of metronidazole reacts with the DNA of a cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Active with respect to Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp., as well as obligate anaerobes Bacteroides spp. (incl. Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella (Prevotella bivia, Prevotella buccae, Prevotella disiens) and some Gram-positive microorganisms (Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp.). The MIC for these strains is 0.125-6.25 μg / ml.

Metronidazole is insensitive to aerobic microorganisms and facultative anaerobes, but in the presence of mixed flora (aerobes and anaerobes) metronidazole acts synergistically with antibiotics effective against conventional aerobes.

Pharmacokinetics:

After a single intravaginal injection of 5 g of Metrogil®, the average maximum concentration of the drug in the serum is 237 ng / ml, which is 2% of the average maximum concentration of metronidazole when administered in a dose of 500 mg.The time to reach the maximum concentration is 6-12 hours after intravaginal application of a single dose of 5 g.

After intravaginal administration, the drug undergoes systemic absorption (about 56%). It penetrates into breast milk and most tissues, passes through the blood-brain barrier and the placenta. The connection with plasma proteins is less than 20%. Metabolized in the liver by hydroxylation, oxidation and glucuronation. Activity of the main metabolite (2-hydroxymethonidazole) - 30% of the activity of the starting compound.

The relative bioavailability of the vaginal gel is 2 times higher than the bioavailability of a single dose (500 mg) of vaginal metronidazole tablets, which is due to the high penetrating ability of the drug in the vaginal fluid. Therefore, the therapeutic effect after intravaginal administration is achieved already at low concentrations of metronidazole.

Indications:

Bacterial vaginosis of different etiology, confirmed by clinical and microbiological data; urogenital trichomoniasis.

Contraindications:

Hypersensitivity (including the derivatives of nitroimidazole), leukopenia (including in the anamnesis), impaired coordination of movements,organic lesions of the central nervous system (including epilepsy), hepatic insufficiency.

Pregnancy - I trimester, lactation.

Pregnancy and lactation:

In the II and III trimesters of pregnancy - only for life indications, when comparing the potential benefits for the mother and the possible risk to the fetus.

Dosing and Administration: ANDintravaginally the recommended dose is 5 g (one complete applicator) 2 times a day (morning and evening). The course of treatment is 5 days.

Side effects:

Local Reactions: burning sensation or frequent urination, vulvitis; a sexual partner - a burning sensation or irritation of the penis.

After the withdrawal of the drug - the development of candidiasis of the vagina.

Possible development system effects: dizziness, headache, dry mouth, taste changes, including "metallic" aftertaste, nausea, vomiting, decreased appetite, abdominal cramps, constipation or diarrhea, dark-colored staining, leukopenia or leukocytosis.

Allergic reactions: skin rash, hives.

In case of any undesirable side effects, stop treatment and consult a doctor!

Overdose:

There were no cases of drug overdose with this method of administration.

Interaction:

Only for intravaginal application!

Similarly, disulfiram causes intolerance ethanol.

Strengthens the action indirect anticoagulants, It is not recommended to combine with nondepolarizing muscle relaxants (vecuronium bromide).

With simultaneous reception with drugs lithium can increase the concentration of lithium in blood plasma.

Phenobarbital accelerates the metabolism of metronidazole due to the induction of microsomal liver enzymes, cimetidine - reduces, which may lead to an increase in its concentration in the serum and an increased risk of side effects.

Special instructions:

Simultaneous treatment of sexual partners is recommended.

During the course of treatment it is necessary to abstain from sexual activity.

With vaginitis caused by Trichomonas vaginalis, it is advisable to simultaneously treat the sexual partner metronidazole for oral administration.

In the case of using the drug in conjunction with metronidazole for oral administration, especially in the second course, control of the picture of peripheral blood (danger of leukopenia) is necessary.

During the period of treatment, alcohol intake is contraindicated (development of a disulfiram-like reaction is possible: spastic abdominal pain, nausea, vomiting, headache, sudden rush of blood to the face).

Metrogyl® can immobilize treponema and lead to Nelson's false positive test.

Form release / dosage:

Vaginal gel, 1%.

Packaging:

- 30 grams per aluminum tube with a protective membrane of aluminum and with a screw cap of polyethylene with a protrusion for perforating the membrane. One tube in a cardboard box together with an applicator and instructions for use.

- 30 grams per plastic laminated tube, sealed with aluminum foil, laminated with polyethylene and with a screw cap made of polypropylene. One tube in a cardboard box together with an applicator and instructions for use.

- 30 grams per plastic laminated tube, sealed with aluminum foil, laminated with polyethylene and with a screw cap of polypropylene with a lip for perforating the foil. One tube in a cardboard box together with an applicator and instructions for use.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:П N011666 / 04

Date of registration:19.01.2009 / 14.07.2009

Expiration Date:Unlimited

The owner of the registration certificate:Unik Pharmaceutical Laboratories Unik Pharmaceutical Laboratories India

Manufacturer: & nbsp

UNIQUE PHARMACEUTICAL Laboratories India

Representation: & nbsp"UNIC PHARMACEUTICAL LABORATORY (branch of the company" JB Chemicals and Pharmaceuticals Ltd. ")""UNIC PHARMACEUTICAL LABORATORY (branch of the company" JB Chemicals and Pharmaceuticals Ltd. ")"India

Information update date: & nbsp11.05.2018

Illustrated instructions

Instructions

Metrogil® (Metrogyl®)